公开(公告)号：US20170114056A1

公开(公告)日：2017-04-27

申请号：US15129206

申请日：2015-03-23

Applicant: Helen MITCHELL ,  Mark E. FRALEY ,  Andrew J. COOKE ,  Craig A. STUMP ,  Yi Heng CHEN ,  Douglas C. BESHORE ,  Xu-Fank ZHANG ,  Casey C. MCCOMAS ,  Kathy SCHIRRIPA ,  Melody MCWHERTER ,  Swati P. MERCER ,  Keith P. MOORE ,  Ping LIU ,  Harold B. WOOD ,  Chun Sing LI ,  Qinghua MAO ,  Merck Sharp & Dohme Corp.

Inventor： Helen Mitchell ,  Mark E. Fraley ,  Andrew J. Cooke ,  Craig A. Stump ,  Yi- Heng Chen ,  Xu-Fang Zhang ,  Casey C. McComas ,  Kathy Schirripa ,  Melody McWherter ,  Swati P. Mercer ,  Keith P. Moore ,  Ping Liu ,  Harold B. Wood ,  Chun Sing Li ,  Qinghua Mao ,  Douglas C. Beshore

IPC: C07D471/04 ,  C07D513/04

CPC classification number: C07D403/12 ,  C07D401/12 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

公开(公告)号：US09499534B2

公开(公告)日：2016-11-22

申请号：US14786466

申请日：2014-04-22

Applicant: Merck Sharp & Dohme Corp.

Inventor： Kenneth L. Arrington ,  Byron DuBois ,  John S. Debenham ,  Ping Liu ,  Alan B. Northrup ,  Jason W. Szewczyk ,  Liping Wang ,  Ming Wang

IPC: C07D417/14 ,  A61K31/427 ,  C07D417/12 ,  A61K31/506 ,  A61K31/5377

CPC classification number: C07D417/14 ,  A61K31/427 ,  A61K31/506 ,  A61K31/5377 ,  C07D417/12

Abstract: The invention provides certain thiazole-substituted aminopyrimidine compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R5, R6, and the subscripts r, s, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).

公开(公告)号：US20230054411A1

公开(公告)日：2023-02-23

申请号：US17294836

申请日：2019-11-26

Applicant: Yonglian ZHANG ,  Amjad ALI ,  Jared CUMMING ,  Duane DEMONG ,  Qiaolin DENG ,  Thomas H. GRAHAM ,  Elisabeth HENNESSY ,  Matthew A. LARSEN ,  Kun LIU ,  Ping LIU ,  Umar Faruk MANSOOR ,  Jianping PAN ,  Christopher W. PLUMMER ,  Aaron SATHER ,  Uma SWAMINATHAN ,  Huijun WANG ,  Merck Sharp & Dohme Corp.

Inventor： Yonglian Zhang ,  Amjad Ali ,  Jared Cumming ,  Duane DeMong ,  Qiaolin Deng ,  Thomas H. Graham ,  Elisabeth Hennessy ,  Matthew A. Larsen ,  Kun Liu ,  Ping Liu ,  Umar Faruk Mansoor ,  Jianping Pan ,  Christopher W. Plummer ,  Aaron Sather ,  Uma Swaminathan ,  Huijun Wang

IPC: A61K31/519 ,  A61K39/395 ,  C07D471/04 ,  C07D519/00 ,  A61K31/55

Abstract: In its many embodiments, the present invention provides certain 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives of Formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A, R1, R2, and R4 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutic agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

公开(公告)号：US10945771B2

公开(公告)日：2021-03-16

申请号：US16620046

申请日：2018-06-04

Applicant: Merck Sharp & Dohme Corp.

Inventor： Dane James Clausen ,  James I. Fells ,  Joseph A. Kozlowski ,  Ping Liu ,  Robert D. Mazzola, Jr.

IPC: A61B17/70 ,  A61B17/17 ,  A61B17/34 ,  A61B17/86 ,  C07D471/04 ,  C07D471/14 ,  C07D498/14 ,  A61B17/56 ,  A61B90/00

Abstract: The present invention is directed to azabicyclo[4.1.0]heptane compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

公开(公告)号：US10556900B2

公开(公告)日：2020-02-11

申请号：US15562617

申请日：2016-04-04

Applicant: Merck Sharp & Dohme Corp.

Inventor： Craig A. Stump ,  Yi Heng Chen ,  Ping Liu ,  Dongfang Meng ,  Jane Yang Wu ,  Chun Sing Li ,  Zhiqi Qi

IPC: C07D471/04 ,  C07D487/04 ,  C07D403/12 ,  C07D417/12 ,  A61P7/02 ,  A61P17/06 ,  A61P9/10 ,  A61P25/00 ,  A61P35/00

Abstract: The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I): which are tropomyos-in-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

公开(公告)号：US10065945B2

公开(公告)日：2018-09-04

申请号：US15104537

申请日：2015-01-20

Applicant: Merck Sharp & Dohme Corp.

Inventor： Richard Berger ,  Timothy A. Blizzard ,  Brian T. Campbell ,  Helen Y. Chen ,  John S. Debenham ,  Sunita V. Dewnani ,  Byron Dubois ,  Candido Gude ,  Zack Zhiqiang Guo ,  Bart Harper ,  Zhiyong Hu ,  Songnian Lin ,  Ping Liu ,  Ming Wang ,  Feroze Ujjainwalla ,  Jiayi Xu ,  Libo Xu ,  Rui Zhang

IPC: C07D413/14 ,  C07D417/14 ,  C07D413/12 ,  C07D471/04 ,  C07D401/12

Abstract: The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

公开(公告)号：US09914736B2

公开(公告)日：2018-03-13

申请号：US15128782

申请日：2015-03-23

Applicant: Merck Sharp & Dohme Corp.

Inventor： Helen Mitchell ,  Mark E. Fraley ,  Andrew J. Cooke ,  Craig A. Stump ,  Xu-Fang Zhang ,  Casey C. McComas ,  Kathy Schirripa ,  Melody McWherter ,  Ping Liu ,  Dann Parker ,  Chun Sing Li ,  Qinghua Mao

IPC: A61K31/40 ,  C07D487/04 ,  C07D277/46 ,  C07D231/40 ,  C07D417/12 ,  C07D401/04 ,  C07D417/14 ,  C07D403/14 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D231/40 ,  C07D277/46 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.